现货大促销,价格低至8折起,量大更优惠,详细咨询客服
全部分类
全部分类
  • Pralatrexate
Pralatrexate的可视化放大

Pralatrexate

A dihydrofolate reductase inhibitor

原价
¥1937-5650
价格
1550-4520
Pralatrexate的二维码

所有产品仅用于科学研究,我们不为任何个人用途提供产品和服务

询价有惊喜,量大更优惠 点击这里给我发消息

  • 库存: 现货
可选包装 >>>
首页
  • 货号: ajci10080
  • CAS: 146464-95-1
  • 别名: 普拉曲沙
  • 分子式: C23H23N7O5
  • 分子量: 477.47
  • 纯度: >98%
  • 溶解度: ≥ 23.85 mg/mL in DMSO
  • 储存: Store at -20°C,protect from light
  • 库存: 现货

Background

Pralatrexate is an inhibitor of DHFR with Ki value of 45 nM [1].


Dihydrofolate reductase (DHFR) is an enzyme that reduces dihydrofolic acid to tetrahydrofolic acid, a methyl group shuttle required for the synthesis of purines, thymidylic acid, and certain amino acids.


Pralatrexate is a DHFR inhibitor with high affinity for folylpolyglutamate synthetase (FPGS) and reduced folate carrier 1 (RFC-1), resulting in extensive internalization and accumulation in tumour cells. In 15 human cancer cell lines, pralatrexate showed antiproliferative effects with IC50 < 0.1 μM in PC3, SCC61, DU145, HT29, HOP62, SQ20B, HOP92, HEP2 and IGROV1 cells. While it showed antiproliferative effects with IC50≥ 9 μM in Colo205, HCC2998, MCF7, HCT116, OVCAR3 and MDA-MB-435 cells [2].


In MV522 human non-small cell lung cancer (NSCLC) xenograft, pralatrexate showed increased antitumor activity. In the 2 mg/kg pralatrexate-treated group, the 38% tumor growth inhibition (TGI) was observed. In NCI-H460 NSCLC xenograft, pralatrexate showed antitumor activity in a dose-dependent way. TGI of 1 mg/kg and 2 mg/kg pralatrexate-treated groups was 34% and 52%, respectively. In the two xenografts, pralatrexate resulted in weight loss, which suggested its toxicity [1].

参考文献:
[1].? Izbicka E, Diaz A, Streeper R, et al. Distinct mechanistic activity profile of pralatrexate in comparison to other antifolates in in vitro and in vivo models of human cancers. Cancer Chemother Pharmacol, 2009, 64(5): 993-999.
[2].? Serova M, Bieche I, Sablin MP, et al. Single agent and combination studies of pralatrexate and molecular correlates of sensitivity. Br J Cancer, 2011, 104(2): 272-280.

Protocol

Cell experiment [1,2]:

Cell lines

Cancer cell lines, NCI-H460 human NSCLC cells, MV522 human metastatic human NSCLC cells

Preparation method

The solubility of this compound in DMSO is > 23.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

72h

Applications

Pralatrexate showed antiproliferative activity against 15 cancer cell lines with the IC50 values ranged from 0.01 ± 0.002 μM for the prostate cancer cell line PC3 to > 350 μM for the MDA-MB-435 cell line. Pralatrexate dose-dependently inhibited the activity of DHFR. In NCI-H460 cells, treatment with pralatrexate for 15 or 60 min resulted in a short-term uptake of radiolabeled antifolates.

Animal experiment [1]:

Animal models

Female nude mice (nu/nu) bearing NCI-H460 or MV522 tumor cells

Dosage form

Intraperitoneal injection, 1 and 2 mg/kg, every day×5, for two cycles of 5 days

Application

In MV522 human non-small cell lung cancer (NSCLC) xenograft, pralatrexate showed increased antitumor activity. In the 2 mg/kg pralatrexate-treated group, the 38% tumor growth inhibition (TGI) was observed. In NCI-H460 NSCLC xenograft, pralatrexate showed antitumor activity in a dose-dependent way. TGI of 1 mg/kg and 2 mg/kg pralatrexate-treated groups was 34% and 52%, respectively. In NCI-H460 and MV522 human tumor xenografts, pralatrexate resulted in dose-dependent weight loss, which suggested its toxicity.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

参考文献:

[1]. Izbicka E, Diaz A, Streeper R, et al. Distinct mechanistic activity profile of pralatrexate in comparison to other antifolates in in vitro and in vivo models of human cancers[J]. Cancer chemotherapy and pharmacology, 2009, 64(5): 993-999.


[2]. Serova M, Bieche I, Sablin M P, et al. Single agent and combination studies of pralatrexate and molecular correlates of sensitivity[J]. British journal of cancer, 2011, 104(2): 272.

动态评分

0.0

没有评分数据
没有评价数据
一键回到顶部
展开 收缩
安捷凯在线客服